Oral Cannabinoid Lipid Formulation for Poor GI Absorption
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Solution Overview
Problem
Oral cannabinoid formulations suffer from sub-optimal absorption, characterized by poor bioavailability, cMax, tMax, and AUC due to poor gastric solubility and metabolism.
Innovation Solution
An oral cannabinoid formulation comprising a cannabinoid component, a long chain triglyceride or fatty acid carrier, and a tocopheryl phosphate component, with specific mass ratios and optionally an aqueous component, to enhance solubility and absorption.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If oral cannabinoid formulations are used, then administration is convenient and preferred for many conditions, but absorption is sub-optimal with poor bioavailability, cMax, tMax, and AUC
Solution Approach 1:
The patent introduces an intermediary substance (lipid carrier such as MCT or LCT) that mediates between the hydrophobic cannabinoid and the aqueous gastric environment. This lipid intermediary solubilizes the cannabinoid, enabling it to interact with the aqueous digestive fluids and be absorbed by the intestinal mucosa, thus resolving the contradiction between ease of oral administration and reliable absorption.
Solution Approach 2:
The patent changes the physical-chemical parameters of the cannabinoid formulation by dissolving it in a lipid carrier, which alters its solubility characteristics. This parameter change (from insoluble in water to soluble in lipid-aqueous interface) enables the cannabinoid to achieve adequate bioavailability, cMax, and AUC while maintaining the convenience of oral administration.
2Ease of operation
If cannabinoids are administered orally, then route is preferred for many conditions, but gastric solubility is poor leading to sub-optimal absorption
Solution Approach 1:
The patent creates a composite material system consisting of cannabinoid dissolved in a lipid carrier (MCT or LCT). This composite formulation combines the hydrophobic cannabinoid with the amphipathic properties of long-chain triglycerides, creating a system that can interface with both the lipid membrane and aqueous gastric environment, thereby achieving adequate solubility while maintaining the preferred oral route of administration.
3Ease of operation
If cannabinoids are administered orally, then convenience is improved, but absorption duration and area under curve are reduced
Solution Approach 1:
The lipid carrier acts as a reservoir and mediator that sustains the release of cannabinoid into the gastrointestinal tract. This intermediary system extends the absorption duration by providing a controlled interface between the cannabinoid and digestive fluids, allowing for prolonged interaction and absorption over time, thus maintaining administration convenience while improving absorption duration and AUC.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
Improves cannabinoid bioavailability by increasing cMax and AUC, providing effective plasma concentrations and therapeutic effects for conditions such as pain, inflammation, and others.
Implementation Method 1
improves the solubility of the cannabinoid in the gastrointestinal tract
Implementation Method 2
a carrier in the form of long chain triglyceride (herein LCT) or long chain fatty acid (herein LCFA)
Data Source
Figure 1A~1B
Figure 1C
Figure 2A~2B
AI summary
The invention relates to an oral cannabinoid formulation comprising: a cannabinoid component comprising a cannabinoid; a carrier in the form of long chain triglyceride (LCT) or long chain fatty acid (LCFA); and a tocopheryl phosphate component comprising mono-(tocopheryl) phosphate (TP) and di-(tocopheryl) phosphate (T2P) wherein the mass ratio of the cannabinoid to the tocopheryl phosphate component is about 10:1 to 1:10.